2. Metabolic Enzyme/Protease Autophagy
  3. Glutaminase Autophagy
  4. Telaglenastat hydrochloride

Telaglenastat hydrochloride  (Synonyms: CB-839 hydrochloride)

目录号: HY-12248A
产品使用指南

摩尔计算器

Telaglenastat (CB-839) hydrochloride 是一种首创的，选择性的，可逆性的，口服活性的谷氨酰胺酶 1 (GLS1) 抑制剂。Telaglenastat hydrochloride 抑制 GLS1 剪接变异体 KGA 和 GAC，比 GLS2 具有更高的选择性。Telaglenastat hydrochloride 对小鼠类肾和脑中的内源性谷氨酰胺酶的 IC50 值分别为 23 nM 和 28 nM。Telaglenastat hydrochloride 还可诱导细胞自噬 (autophagy)，并具有强大的抗肿瘤活性。

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Telaglenastat hydrochloride Chemical Structure

Telaglenastat hydrochloride Chemical Structure

CAS No. : 1874231-60-3

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Telaglenastat hydrochloride 的其他形式现货产品:

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Other Forms of Telaglenastat hydrochloride:

Telaglenastat hydrochloride 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 57 篇科研文献

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Proliferation Assay

    Telaglenastat hydrochloride purchased from MCE. Usage Cited in: Pathol Int. 2023 Feb 24.  [Abstract]

    Telaglenastat (1, 2.5, 5, 10 μM; 5 days) inhibits the proliferation of DeGISTL1 cells dose-dependently.

    Telaglenastat hydrochloride purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Jun;40(6):814-822.  [Abstract]

    The protein expression levels of the genes related to cell cycle and metabolism are detected by immunoblotting using the corresponding antibodies in H1299 cells treated with 20 nM THZ1 alone or in combination with 500 nM CB-839 for 48 h.

    Telaglenastat hydrochloride purchased from MCE. Usage Cited in: Am J Respir Cell Mol Biol. 2018 Mar;58(3):378-390.  [Abstract]

    Human normal lung fibroblasts are treated as in A. Levels of the indicated proteins are determined by Western blotting. CB-839 remarkably inhibits the expression of Collagens I and III in myofibroblasts.

    Telaglenastat hydrochloride purchased from MCE. Usage Cited in: Biochem Biophys Res Commun. 2018 Oct 2;504(2):415-421.  [Abstract]

    PC3 cells are treated with indicated doses of CB-839 for 24 h after c-Myc overexpression. Cells are then harvested for the determination of indicated proteins levels.

    Telaglenastat hydrochloride purchased from MCE. Usage Cited in: Cancer Discov. 2017 Apr;7(4):380-390.  [Abstract]

    MEFs treated with 12.5 nM CB-839 or control (one-way ANOVA).

    Telaglenastat hydrochloride purchased from MCE. Usage Cited in: Blood Adv. 2017 Jul 14;1(17):1296-1305.  [Abstract]

    The drug could be detected through MS only in the plasma from rats receiving its administration, confirming its systemic bioavailability after the treatment. Labeling scheme in panels B and C is based on the presence (+) or absence (−) of shock, DMSO (control for vehicle to the drug CB-839), and glutaminase inhibitor. Three columns are graphed per each group, indicating baseline, postshock, and end-of-shock values.

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity[1].

    体外研究
    (In Vitro)

    Telaglenastat (CB-839) (0.1-1000 nM; 72 hours) has antiproliferative activity in HCC1806 and MDA-MB-231 cells with IC50s of 49 nM and 26 nM, respectively[1].
    Telaglenastat (CB-839) (1 μM; 72 hours) activates caspase 3/7 and induces apoptosis in MDA-MB-231 and HCC1806 cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Telaglenastat hydrochloride 相关抗体:

    Cell Proliferation Assay[1]

    Cell Line: HCC1806, MDA-MB-231 cells
    Concentration: 0.1, 1, 10, 100, 1000 nM
    Incubation Time: 72 hours
    Result: Has a potent effect on the proliferation of the two TNBC cell lines (IC50 of 49 nM and 26 nM for HCC1806 and MDA-MB-231 cells).

    Apoptosis Analysis[1]

    Cell Line: MDA-MB-231, HCC1806 cells
    Concentration: 1 μM
    Incubation Time: 72 hours
    Result: Caspase 3/7 activation.
    体内研究
    (In Vivo)

    Telaglenastat (CB-839) (200 mg/kg; p.o.; twice daily for 28 days) has antitumor activity in xenograft models of TNBC[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Model: Female nu/nu mice with age 4–6 weeks (TNBC patient-derived xenograft model)[1]
    Dosage: 200 mg/kg
    Administration: Oral administration; twice daily for 28 days
    Result: Suppressed tumor growth by 61% relative to vehicle control at the end of study.
    Clinical Trial
    分子量

    608.04

    Formula

    C26H25ClF3N7O3S
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Telaglenastat hydrochloride 相关分类

    • 摩尔计算器

    • 稀释计算器

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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Telaglenastat1874231-60-3CB-839CB839CB 839GlutaminaseAutophagyselectivetriple-negativebreastcancerTNBCantiproliferativeHCC-1806PDACcellsplicevariantsInhibitorinhibitorinhibit

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